[CAS NO. 575474-82-7] R112
PRODUCTS SPECIFICATIONS [575474-82-7]
DESCRIPTION [575474-82-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 312.30 |
| Molecular Formula | C16H13FN4O2 |
| SMILES | FC1=CN=C(NC2=CC(O)=CC=C2)N=C1NC3=CC(O)=CC=C3 |
Summary
IC50 & Target
IC50: 226 nM (Syk kinase) [1]
In Vitro
R112 (0.001-10 μM; 1 h) dose-dependently inhibits anti-IgE-mediated tryptase release and histamine release with EC
50
s of 0.353 and 0.28 μM, inhibits histamine release by basophils stimulated with an EC
50
value of 0.49 μM, inhibits secretion of LTC4, TNF-α, GM-CSF and IL-8 with EC
50
s of 0.115, 2.01, 1.58 and 1.75 μM, respectively
[1]
.
R112 (0-10 μM; 40 min) inhibits Syk target LAT (Y191) phosphorylation
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | Human mast cells |
| Concentration: | 0.4, 2 and 10 μM |
| Incubation Time: | 40 min |
| Result: | Inhibited phosphorylation of the Syk target LAT (Y191) and also inhibited phosphorylation of Syk downstream events. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 55 mg/mL ( 176.11 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2020 mL | 16.0102 mL | 32.0205 mL |
| 5 mM | 0.6404 mL | 3.2020 mL | 6.4041 mL |
| 10 mM | 0.3202 mL | 1.6010 mL | 3.2020 mL |